Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor (IC50s: 0.3 nM and 1.4 nM, respectively).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 45,800 | 10-14周 | ||
50 mg | ¥ 61,800 | 10-14周 | ||
100 mg | ¥ 86,500 | 10-14周 |
产品描述 | PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor (IC50s: 0.3 nM and 1.4 nM, respectively). |
靶点活性 | RLK:1.4 nM, BLK:125 nM, BTK:17 nM, JAK3:30 nM, BMX:17 nM, ITK:0.3 nM, TEC:3.3 nM |
体外活性 | PRN694 obviously decreases NK cell FcR-induced killing at concentrations exceeding 0.37 μM. PRN694 inhibits TEC, BTK, BMX, BLK, JAK3 with IC50s of 3.3, 17, 17, 125, 30 nM, respectively. Immunoblot analysis of TCR activation pathways shows that PRN694 blocks activation or nuclear translocation of NFAT1, JunB, pIκBα, and pERK. Results display inhibition of Ca2+ signaling with PRN694 at all concentrations above 1 nM. Day 6 flow cytometry analysis reveals that PRN694 significantly inhibits the anti-CD3/CD28-induced proliferation of both CD4 and CD8 T-cells (p<0.01)[1]. |
体内活性 | RN694 treatment also causes obviously lower weights relative to the vehicle (p<0.05). Colitis studies show reduced numbers of CD4+ T cells present in the colonic epithelium of PRN694-treated mice compare with controls. The PRN694 occupancy of ITK is 98, 95, and 54% at 1, 6, and 14 h, respectively. The concentrations of PRN694 in the plasma are 2.8, 0.66, and 0.027 μM at 1, 6, and 14 h, respectively. At 14 h, the plasma level of PRN694 is over 10 fold lower than the IC50 in whole blood [1][2]. |
分子量 | 543.67 |
分子式 | C28H35F2N5O2S |
CAS No. | 1575818-46-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (229.92 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8394 mL | 9.1968 mL | 18.3935 mL | 45.9838 mL |
5 mM | 0.3679 mL | 1.8394 mL | 3.6787 mL | 9.1968 mL | |
10 mM | 0.1839 mL | 0.9197 mL | 1.8394 mL | 4.5984 mL | |
20 mM | 0.092 mL | 0.4598 mL | 0.9197 mL | 2.2992 mL | |
50 mM | 0.0368 mL | 0.1839 mL | 0.3679 mL | 0.9197 mL | |
100 mM | 0.0184 mL | 0.092 mL | 0.1839 mL | 0.4598 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PRN694 1575818-46-0 Others PRN 694 PRN-694 Inhibitor inhibitor inhibit